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1. 发明授权

US4304715A Enkephalin analogues 失效
标题翻译：脑啡肽类似物
公开(公告)号：US4304715A
公开(公告)日：1981-12-08
申请号：US112122
申请日：1980-01-14
申请人： Derek Hudson , Robert Sharpe , Michael Szelke
发明人： Derek Hudson , Robert Sharpe , Michael Szelke
IPC分类号： A61K38/17 , C07K5/00 , C07K5/02 , C07K5/065 , C07K5/083 , C07K5/087 , G01N33/53 , C07C103/52
CPC分类号： C07K5/06078 , C07K5/0207 , C07K5/0804 , C07K5/0812 , Y10S514/809
摘要： Compounds corresponding in structure to enkephalin or polypeptide analogues thereof, wherein one or more peptide links of the enkephalin or analogue is represented by a group or groups the same or different selected from dimethylene, hydroxydimethylene, methylene-imino and ketomethylene groups and/or wherein adjacent peptide bond nitrogen atoms are linked by a carbonyl or thiocarbonyl group.
摘要翻译：结构相对于脑啡肽或其多肽类似物的化合物，其中脑啡肽或类似物的一个或多个肽连接由选自二亚甲基，羟基二亚甲基，亚甲基亚氨基和酮亚甲基的基团或基团表示，和/或其中相邻肽键氮原子通过羰基或硫代羰基连接。

2. 再颁专利

USRE30731E Enkephalin analogues 失效
标题翻译：脑啡肽类似物
公开(公告)号：USRE30731E
公开(公告)日：1981-09-01
申请号：US178345
申请日：1980-08-14
申请人： Derek Hudson , Robert Sharpe , Michael Szelke
发明人： Derek Hudson , Robert Sharpe , Michael Szelke
IPC分类号： A61K38/00 , C07C271/22 , C07K5/02 , C07K14/70
CPC分类号： C07C271/22 , C07K14/702 , C07K5/0207 , A61K38/00 , Y10S514/809
摘要： Compounds corresponding in structure to enkephalin or polypeptide analogues thereof, wherein one or more peptide links of the enkephalin or analogue is represented by a group or groups the same or different selected from dimethylene, methylene-imino and keto-methylene groups.

3. 发明授权

US4198398A Enkephalin analogues 失效
标题翻译：脑啡肽类似物
公开(公告)号：US4198398A
公开(公告)日：1980-04-15
申请号：US923478
申请日：1978-07-10
申请人： Derek Hudson , Robert Sharpe , Michael Szelke
发明人： Derek Hudson , Robert Sharpe , Michael Szelke
IPC分类号： A61K38/00 , C07C271/22 , C07K5/02 , C07K14/70 , A61K37/00 , C07C103/52
CPC分类号： C07C271/22 , C07K14/702 , C07K5/0207 , A61K38/00 , Y10S514/809
摘要： Compounds corresponding in structure to enkephalin or polypeptide analogues thereof, wherein one or more peptide links of the enkephalin or analogue is represented by a group or groups the same or different selected from dimethylene, methylene-imino and keto-methylene groups.
摘要翻译：结构相应于脑啡肽或其多肽类似物的化合物，其中脑啡肽或类似物的一个或多个肽连接由选自二亚甲基，亚甲基亚氨基和酮 - 亚甲基的基团或基团表示。

4. 发明授权

US06277957B1 Method for production of acylthio derivatives 失效
标题翻译：酰基硫代衍生物的制备方法
公开(公告)号：US06277957B1
公开(公告)日：2001-08-21
申请号：US09533095
申请日：2000-03-23
申请人： Derek Hudson , Stewart Thompson
发明人： Derek Hudson , Stewart Thompson
IPC分类号： C07C32720
CPC分类号： C07K1/1077 , C07C327/22 , C07K1/086
摘要： A method is provided which facilitates and enables the production of a wide range of complex conjugates composed of similar or dissimilar units linked together by amide bonds. Said method for the production of acylthio derivatives, R′—CO—SA, involves reaction of a carboxylate, R′—CO—O− (or carboxylic acid R′—CO—OH) with an iso-thiouronium derivative (bearing SA) in the presence of base. Nucleophilic counterion forms of the iso-thiouronium salts confer significant rate enhancement. The processes are simple, generally applicable, efficient, and do not require the employment of noxious reagents. The production of complex protein-like products by the intermediary of acylthio esters generated by the process of this invention, provides a method which is compatible with mild methods of chain assembly; and is preferably applied when the second component in the ligation bears an amino terminal cysteine residue.
摘要翻译：提供了一种方法，其促进并使得能够生产由通过酰胺键连接在一起的相似或不同单元组成的多种复合共轭体。所述制备酰基硫代衍生物R'-CO-SA的方法包括羧酸酯R'-CO-O-（或羧酸R'-CO-OH）与异硫脲衍生物（带有SA）反应，在基地的存在下。异硫脲鎓盐的亲核抗衡离子形式具有显着的速率增加。这些方法简单，一般适用，高效，不需要使用有毒试剂。通过本发明方法产生的酰基硫代酯的中间产生复杂的蛋白质样产物提供了一种与温和的链组装方法相容的方法; 并且优选在连接中的第二组分具有氨基末端半胱氨酸残基时应用。

5. 发明授权

US5233044A Active esters for solid phase peptide synthesis 失效
标题翻译：用于固相肽合成的活性酯
公开(公告)号：US5233044A
公开(公告)日：1993-08-03
申请号：US766895
申请日：1991-09-26
申请人： Derek Hudson
发明人： Derek Hudson
IPC分类号： C07D231/22 , C07K1/08 , C07K1/10
CPC分类号： C07K1/084 , C07D231/22 , C07K1/10
摘要： Derivatives of 1-phenyl pyrazolin-5-one have many applications for biomolecule synthesis. Enol esters of protected amino acids made by the present process provide efficient coupling in solid-phase peptide synthesis. The 1-phenyl-pyrazolin-5-one derivatives are highly crystalline, stable, non-toxic and easy to prepare. Many possess self-indicating properties, facilitating spectrophotometric monitoring and automation of peptide synthesis.
摘要翻译： 1-苯基吡唑啉-5-酮的衍生物具有生物分子合成的许多应用。通过本方法制备的受保护氨基酸的烯醇酯在固相肽合成中提供有效的偶联。 1-苯基 - 吡唑啉-5-酮衍生物高度结晶，稳定，无毒，易于制备。许多具有自我指示性质，促进分光光度监测和肽合成的自动化。

6. 发明授权

US5147608A Apparatus and process for performing repetitive chemical processing 失效
标题翻译：执行重复化学处理的装置和方法
公开(公告)号：US5147608A
公开(公告)日：1992-09-15
申请号：US188453
申请日：1988-04-29
申请人： Derek Hudson , Jordan Honig , Ronald M. Cook , Douglas J. Ng
发明人： Derek Hudson , Jordan Honig , Ronald M. Cook , Douglas J. Ng
IPC分类号： C07H21/04 , B01J19/00 , C07K1/04 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00
CPC分类号： C07K1/045 , B01J19/0046 , B01J2219/00286 , B01J2219/0029 , B01J2219/005 , B01J2219/00549 , B01J2219/0059 , B01J2219/00596 , B01J2219/00686 , B01J2219/00725 , B01J2219/00731 , C40B40/10 , C40B40/12 , C40B60/14 , C40B70/00 , Y10T436/11
摘要： A chemical processing system is disclosed for the automated dissolution, dispersing and reaction of chemicals, especially for synthesizing proteins. The system includes a plurality of storage cartridges containing a first chemical in fluid communication with a reservoir containing a second chemical to be reacted with the first chemical. Each cartridge includes a pump (e.g., a plunger) which operates by changing the internal volume of the cartridge. The pump permits bi-directional flow of the first chemical into and out of the reservoir and cartridge to promote mixing and reacting with the second chemical in the reservoir to produce a third chemical.

7. 发明授权

US5591646A Method and apparatus for peptide synthesis and screening 失效
标题翻译：肽合成和筛选的方法和装置
公开(公告)号：US5591646A
公开(公告)日：1997-01-07
申请号：US939065
申请日：1992-09-02
申请人： Derek Hudson , Charles R. Johnson , Lutz Giebel
发明人： Derek Hudson , Charles R. Johnson , Lutz Giebel
IPC分类号： B01D61/18 , B01J19/00 , B01L3/00 , C07K1/04 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , G01N33/543 , C07K17/00
CPC分类号： B01L3/5025 , B01D61/18 , B01J19/0046 , B01L3/50255 , C07K1/045 , C07K1/047 , B01J2219/00416 , B01J2219/0043 , B01J2219/00497 , B01J2219/005 , B01J2219/00527 , B01J2219/00531 , B01J2219/00536 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/00617 , B01J2219/00619 , B01J2219/00626 , B01J2219/00641 , B01J2219/00659 , B01J2219/00664 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01J2219/00731 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , Y02P20/582
摘要： Method and apparatus for simple and rapid preparation of reusable, addressable surface-immobilized arrays of biomolecules (libraries) used for screening for interaction with any biologically significant target. A special plate having on its surface a plurality of discreet functionalized substrate areas, typically in arrays of 10.times.10 to 400.times.400, is provided for chemical synthesis or bonding thereon of desired families of biomolecules (e.g. peptides, DNA, RNA, oligosaccharides). In the case of peptides, such as hexapeptides, the resulting permanently hexapeptide-loaded plate is a reusable Addressable Synthetic Peptide Combinatorial Library (ASPCL), in which 1 to 3 (typically two) of the positions in the sequence are uniquely identified by the address location. Plate embodiments include substrates of physically bonded (e.g. glued) conventional particulate materials such as Pepsyn-K, or functionalizable films of linear or crosslinked polymers covalently attached to, or physically adhered to the plate surface. Spacer arm moieties may also be attached to the substrates. A unique multi-slot block assembly is used to prepare the ASPCLs. In library applications, for example determining peptides which bind to functional proteins (enzymes, receptors, antibodies), the substrate-bound peptides are assembled with several positions consisting of uniformly distributed equimolar mixtures of residues, and 2 separated or sequential positions uniquely identified by their spatial location on the substrate array, the "address". Following identification of the known residues giving the greatest affinity for the arrayed positions in the sequence, optimal binding for the complete peptide sequence is determined by an iterative process replacing formerly mixed positions with known AAs at unique addresses.
摘要翻译：用于简单快速地制备用于筛选与任何生物学显着靶物相互作用的生物分子（文库）的可重复使用的，可寻址的表面固定化阵列的方法和装置。在其表面上具有通常为10×10 -4 400×400阵列的多个离散的官能化底物区域的特殊板，用于化学合成或在其上键合所需要的生物分子族（例如肽，DNA，RNA，寡糖）。在肽（例如六肽）的情况下，所得到的永久性六肽加载的板是可重复使用的可寻址合成肽组合文库（ASPCL），其中序列中的1至3个（通常为2个）位置由地址唯一地标识位置。板实施方案包括物理结合（例如胶合）常规颗粒材料如Pepsyn-K的基材或共价附着或物理粘附到板表面的线性或交联聚合物的官能化膜。间隔臂部分也可以附着到基底上。使用独特的多槽块组件来准备ASPCL。在文库应用中，例如确定与功能蛋白（酶，受体，抗体）结合的肽，底物结合的肽由几个位置组成，其中包含均匀分布的等摩尔残基混合物，以及由它们独特地鉴定的2个分离或连续位置衬底阵列上的空间位置，“地址”。在鉴定对序列中的排列位置具有最大亲和性的已知残基之后，通过迭代过程来确定完整肽序列的最佳结合，该迭代过程将以前与独特地址的已知AAs混合的位置替换。

8. 发明授权

US5585275A Pilot apparatus for peptide synthesis and screening 失效
标题翻译：用于肽合成和筛选的试验装置
公开(公告)号：US5585275A
公开(公告)日：1996-12-17
申请号：US79741
申请日：1993-06-18
申请人： Derek Hudson , Charles R. Johnson , Lutz Giebel
发明人： Derek Hudson , Charles R. Johnson , Lutz Giebel
IPC分类号： B01D61/18 , B01J19/00 , B01L3/00 , C07K1/04 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , G01N33/543 , C07K17/00
CPC分类号： B01L3/5025 , B01D61/18 , B01J19/0046 , B01L3/50255 , C07K1/045 , C07K1/047 , B01J2219/00416 , B01J2219/0043 , B01J2219/00459 , B01J2219/00497 , B01J2219/005 , B01J2219/00527 , B01J2219/00531 , B01J2219/00536 , B01J2219/00585 , B01J2219/0059 , B01J2219/00596 , B01J2219/00605 , B01J2219/0061 , B01J2219/00612 , B01J2219/00617 , B01J2219/00619 , B01J2219/00626 , B01J2219/00641 , B01J2219/00659 , B01J2219/00664 , B01J2219/0072 , B01J2219/00722 , B01J2219/00725 , B01J2219/00731 , C40B40/06 , C40B40/10 , C40B40/12 , C40B60/14 , Y02P20/582
摘要： Method and apparatus for simple and rapid preparation of reusable, addressable surface-immobilized arrays of biomolecules (libraries) used for screening for interaction with any biologically significant target. A special plate having on or in its surface a plurality of discreet functionalized substrate areas, typically in arrays of 10.times.10 to 400.times.400, is provided for chemical synthesis or bonding thereon of desired families of biomolecules (e.g. peptides, DNA, RNA, oligosaccharides). In the case of peptides, such as hexapeptides, the resulting permanently hexapeptide-loaded plate is a reusable Addressable Synthetic Peptide Combinatorial Library (ASPCL), in which 1 to 3 (typically two) of the positions in the sequence are uniquely identified by the address location. The preferred plate embodiment employs an HPMP wink of porous polyolefin removably received in holes in the plate. A unique multi-slot block assembly is used to prepare the ASPCLs. The wink carrier plate is also employed with a vacuum block system to assist in washing, deprotection, and probing. In library applications, for example determining peptides which bind to functional proteins (enzymes, receptors, antibodies), the substrate-bound peptides are assembled with several positions consisting of uniformly distributed equimolar mixtures of residues, and 2 separated or sequential positions uniquely identified by their spatial location on the substrate array, the "address". Following identification of the known residues giving the greatest affinity for the arrayed positions in the sequence, optimal binding for the complete peptide sequence is determined by an iterative process replacing formerly mixed positions with known AAs at unique addresses.
摘要翻译：用于简单快速地制备用于筛选与任何生物学显着靶物相互作用的生物分子（文库）的可重复使用的，可寻址的表面固定化阵列的方法和装置。在其上或其表面上具有通常为10×10 -4 400×400阵列的多个离散功能化底物区域的特殊板被提供用于化学合成或在其上键合所需要的生物分子族（例如肽，DNA，RNA，寡糖）。在肽（例如六肽）的情况下，所得到的永久性六肽加载的板是可重复使用的可寻址合成肽组合文库（ASPCL），其中序列中的1至3个（通常为2个）位置由地址唯一地标识位置。优选的板实施例使用可拆卸地容纳在板中的孔中的多孔聚烯烃的HPMP眨眼。使用独特的多槽块组件来准备ASPCL。眨眼承载板也与真空块系统一起使用以帮助洗涤，去保护和探测。在文库应用中，例如确定与功能蛋白（酶，受体，抗体）结合的肽，底物结合的肽由几个位置组成，其中包含均匀分布的等摩尔残基混合物，以及由它们独特地鉴定的2个分离或连续位置衬底阵列上的空间位置，“地址”。在鉴定对序列中的排列位置具有最大亲和性的已知残基之后，通过迭代过程来确定完整肽序列的最佳结合，该迭代过程将以前与独特地址的已知AAs混合的位置替换。

9. 发明授权

US4935536A Protecting groups for asparagine and glutamine in peptide synthesis 失效
标题翻译：肽合成中天冬酰胺和谷氨酰胺的保护基
公开(公告)号：US4935536A
公开(公告)日：1990-06-19
申请号：US316570
申请日：1989-02-27
申请人： Derek Hudson
发明人： Derek Hudson
IPC分类号： C07K1/06
CPC分类号： C07K1/066 , Y02P20/55
摘要： Trialkoxybenzyl (Taob) protected asparagine and glutamine, a method of synthesis and a method of use are provided. The Taob protected Asn and Gln have the following formulae: ##STR1## wherein Z is an alkyl group having from 1 to 10 carbon atoms; X and W are any .alpha.-protecting group which can be selectively removed while maintaining Taob intact; Y is H or any group sufficiently active or activatable to react with NH.sub.2 -- or NH.dbd. to generate an amide bond; n is 1 for asparagine or 2 for glutamine. These derivatives are stable in solution, have good solubility in organic solvents and couple directly without side reactions.
摘要翻译：提供三烷氧基苄基（Taob）保护的天冬酰胺和谷氨酰胺，合成方法和使用方法。 Taob保护的Asn和Gln具有下式：其中Z是具有1至10个碳原子的烷基; X和W是任何α保护基团，可以选择性地去除，同时保持Taob完整; Y是H或足够活性或可活化以与NH 2 - 或NH 3反应以产生酰胺键的任何基团; 天冬酰胺n为1，谷氨酰胺为2。这些衍生物在溶液中是稳定的，在有机溶剂中具有良好的溶解性并直接偶联而无副反应。

10. 发明授权

US4474947A Benzazolides and their employment in phosphate ester oligonucleotide synthesis processes 失效
标题翻译：苯并唑啉及其在磷酸酯寡核苷酸合成过程中的应用
公开(公告)号：US4474947A
公开(公告)日：1984-10-02
申请号：US366537
申请日：1982-04-08
申请人： Derek Hudson , Ronald M. Cook
发明人： Derek Hudson , Ronald M. Cook
IPC分类号： C07D235/08 , C07D249/18 , C07F9/6506 , C07F9/6518 , C07H21/00 , C07H19/10
CPC分类号： C07H21/00 , C07D235/08 , C07D249/18 , C07F9/65068 , C07F9/65188
摘要： Benzazoles, including benzatriazoles and benzimidazoles are employed in phospate triester oligonucleotide synthesis. The benzazoles form arylbenzazolide coupling agents, and phosphorodibenzazolides. Processes employing these reagents are also disclosed.
摘要翻译：苯并唑，包括苯并三唑和苯并咪唑，用于磷酸三酯寡核苷酸合成。苯并唑形成芳基苯并唑化偶合剂和磷酰苯并唑。还公开了使用这些试剂的方法。

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